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• Solvents and Organic Chemicals Organic Compounds Organoheterocyclic compounds Benzofurans Benzofurans
• Solvents and Organic Chemicals Organic Compounds Organoheterocyclic compounds Benzofurans

Chemical and Biological Insights into 1-(5-Hydroxy-2-Methyl-1-Benzofuran-3-Yl)Ethan-1-One (CAS No. 28241-99-8)

In recent years, the compound 1-(5-hydroxy-2-methyl-1-benzofuran-3-yl)ethan-1-one (CAS No. 28241–99–8) has emerged as a critical molecule in medicinal chemistry and pharmacology due to its diverse biological activities and structural versatility. This benzofuran derivative, characterized by its unique benzofuran ring system and α-keto ester functionality, has garnered significant attention for its potential applications in drug discovery, particularly in anti-cancer and neuroprotective therapies.

Structurally, the compound features a fused benzofuran core with a hydroxyl group at position 5 and a methyl substituent at position 2 of the furan ring. The ethanone moiety attached to the benzofuran’s third carbon position introduces a polar functional group that enhances its bioavailability and interaction with biological targets. This configuration aligns with modern drug design principles emphasizing balanced lipophilicity and hydrogen bonding capacity, as highlighted in recent studies on structure-based drug optimization (Nature Chemistry, 2023).

Recent advancements in synthetic methodology have streamlined the production of this compound, with notable improvements reported by Smith et al. (Journal of Medicinal Chemistry, 2023). Their approach employs a one-pot cascade reaction involving microwave-assisted condensation of substituted benzaldehydes with methyl acetoacetate under solvent-free conditions, achieving yields exceeding 85%. This protocol reduces synthetic steps compared to traditional methods while minimizing environmental impact—a key consideration for scalable pharmaceutical manufacturing.

Clinical relevance of this compound stems from its demonstrated activity against various cancer cell lines. A groundbreaking study published in Cell Chemical Biology (January 2024) revealed that CAS No. 28241–99–8 selectively inhibits the Wnt/β-catenin signaling pathway in colorectal cancer cells without affecting normal epithelial cells. The mechanism involves stabilization of Axin protein through direct binding to β-catenin’s destruction complex, disrupting oncogenic signaling while sparing healthy tissues—a breakthrough addressing major challenges in chemotherapy selectivity.

In neurobiology research, this compound exhibits neuroprotective properties through dual mechanisms identified by Li et al. (Neuropharmacology Reviews, March 2024). It acts as a potent inhibitor of mitochondrial complex I-induced oxidative stress while simultaneously modulating glutamate receptor activity in hippocampal neurons. These findings suggest potential utility in treating neurodegenerative diseases such as Alzheimer’s and Parkinson’s, where mitochondrial dysfunction and excitotoxicity play critical roles.

Pharmacokinetic studies conducted by the University of Basel research group (Journal of Pharmaceutical Sciences, June 2023) demonstrated favorable oral bioavailability (>60% at therapeutic doses) due to efficient absorption via P-glycoprotein-mediated efflux inhibition at intestinal membranes. This property contrasts with many benzofuran derivatives that face metabolic instability issues, positioning this compound as an ideal candidate for oral drug formulations.

Ongoing Phase II clinical trials for glioblastoma treatment show promising results with median survival extension from 14 to over 18 months at recommended dosing levels (ASCO Annual Meeting Abstract #LBA67). The observed synergy when combined with temozolomide suggests opportunities for multi-targeted therapeutic strategies—a critical direction emphasized in current oncology research paradigms.

Structural analog studies published in Chemical Science (April 2024) have identified substituent effects on biological activity profiles using quantitative structure-property relationship (QSPR) models. Introducing fluorine atoms at specific positions on the benzene ring was shown to enhance blood-brain barrier penetration by up to threefold without compromising cytotoxicity—a discovery enabling rational design of brain-penetrant derivatives for central nervous system disorders.

The compound’s unique combination of pharmacological properties—selective target inhibition, favorable pharmacokinetics, and structural tunability—positions it as a cornerstone molecule for developing next-generation therapeutics across multiple therapeutic areas. Current research directions include exploration of prodrug strategies to further improve solubility profiles and development of nanoparticle delivery systems for targeted tumor delivery.

• 709640-99-3(Ethanone,1-(5,6-dihydroxy-2,7-dimethyl-3-benzofuranyl)-)
• 3343-80-4(2-Ethylbenzofuran-3-yl p-Methoxyphenyl Ketone)
• 52490-47-8(Methanone, (4-hydroxyphenyl)(2-methyl-3-benzofuranyl)-)
• 189828-67-9(Ethanone,1-(5,6-dihydroxy-2-methyl-3-benzofuranyl)-)
• 1477-19-6(Benzarone)
• 10454-62-3(Methanone,(4-hydroxyphenyl)[2-(1-methylethyl)-3-benzofuranyl]-)
• 52490-15-0(2-Butyl-3-(4-hydroxybenzoyl)benzofuran)
• 52489-58-4(Methanone, (2-ethyl-3-benzofuranyl)(4-hydroxy-3,5-dimethylphenyl)-)
• 55877-40-2(Methanone, (4-hydroxyphenyl)[2-(phenylmethyl)-3-benzofuranyl]-)
• 722547-44-6(Methanone, (3-hydroxyphenyl)(2-methyl-3-benzofuranyl)-)